878231-90-4Relevant academic research and scientific papers
Identification of a novel spiropiperidine opioid receptor-like 1 antagonist class by a focused library approach featuring 3D-pharmacophore similarity
Goto, Yasuhiro,Arai-Otsuki, Sachie,Tachibana, Yukari,Ichikawa, Daisuke,Ozaki, Satoshi,Takahashi, Hiroyuki,Iwasawa, Yoshikazu,Okamoto, Osamu,Okuda, Shoki,Ohta, Hisashi,Sagara, Takeshi
, p. 847 - 849 (2007/10/03)
A focused library approach identifying novel leads to develop a potent ORL1 antagonist is described. Beginning from a compound identified by random screening, an exploratory library that exhibited a diverse display of pharmacophores was designed. After evaluating ORL1 antagonistic activity, a highly focused library was designed based on 3D-pharmacophore similarity to known actives. A novel D-proline amide class was identified in this library and was found to possess potent ORL1 antagonistic activity.
